Tankyrase-IN-2

Modify Date: 2024-01-15 12:05:50

Tankyrase-IN-2 Structure
Tankyrase-IN-2 structure
Common Name Tankyrase-IN-2
CAS Number 1588870-36-3 Molecular Weight 316.30
Density N/A Boiling Point N/A
Molecular Formula C17H14F2N2O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Tankyrase-IN-2


Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model[1].

 Names

Name Tankyrase-IN-2

 Tankyrase-IN-2 Biological Activity

Description Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model[1].
Related Catalog
Target

IC50: 10 nM (TNKS1), 7 nM (TNKS2), 710 nM (PARP1)[1]

In Vitro Tankyrase-IN-2 (1-10000 nM; 24 hours) leads to a dose-dependent increase of tankyrase protein abundance with an EC50 of 320 nM in DLD1 cells. This is in the same potency range as the value for axin2 increase (EC50=319 nM)[1].
References

[1]. Buchstaller HP, et al. Discovery and Optimization of 2-Arylquinazolin-4-ones into a Potent and Selective TankyraseInhibitor Modulating Wnt Pathway Activity. J Med Chem. 2019 Aug 5.

 Chemical & Physical Properties

Molecular Formula C17H14F2N2O2
Molecular Weight 316.30